Cafestol, a diterpene molecule found in coffee, induces leukemia cell death

Lima, Cristiano de; Spindola, Daniel Gonsales; Bechara, Alexandre Henrique Silveira; Garcia, Daniel M.; Palmeira-dos-Santos, Caroline; Peixoto-da-Silva, Janaína; Erustes, Adolfo Garcia; Michelin, Luis Felipe Gomes; Pereira, Gustavo José da Silva; Smaili, Soraya Soubhi; Paredes‐Gamero, Edgar Julian; Calgarotto, Andrana K.; Oliveira, Carlos Rocha; Bincoletto, Cláudia

doi:10.1016/j.biopha.2017.05.109

Cited by 28 publications

(13 citation statements)

References 33 publications

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“…Bcl-2 family proteins are both activators and inhibitors, playing a pivotal role in the process of apoptosis. Another marker of the apoptotic pathway is the cleavage of caspase-3, which is the most important terminal cleavage enzyme in apoptosis [52].…”

Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

“…Lee et al [55] considered that cafestol (30–90 μM) and kahweol (20–60 μM) suppressed Sp1 protein expression to down-regulate apoptotic proteins through a study on human malignant pleural mesothelioma. Recently, Lima et al [52] have found that cafestol (80 μM) can reduce the production of ROS in the leukemia cell line HL60. Moreover, the differentiation markers CD11b and CD15 increase with cafestol treatment at low doses (10 μM).…”

Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

“…According to previous studies, cafestol effectively overcomes the resistance to ABT-737 of human glioma U251MG cells and human breast carcinoma MDA-MB231 cells [54]. The combination of cafestol and Ara-C reduced the viability of HL60 cells more efficiently compared with the two drugs used alone [52]. Kahweol and sorafenib showed a synergistic effects in inducing apoptosis on Caki cells [71].…”

Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

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Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Ren

Wang

et al. 2019

IJMS

103

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Cafestol and kahweol are natural diterpenes extracted from coffee beans. In addition to the effect of raising serum lipid, in vitro and in vivo experimental results have revealed that the two diterpenes demonstrate multiple potential pharmacological actions such as anti-inflammation, hepatoprotective, anti-cancer, anti-diabetic, and anti-osteoclastogenesis activities. The most relevant mechanisms involved are down-regulating inflammation mediators, increasing glutathione (GSH), inducing apoptosis of tumor cells and anti-angiogenesis. Cafestol and kahweol show similar biological activities but not exactly the same, which might due to the presence of one conjugated double bond on the furan ring of the latter. This review aims to summarize the pharmacological properties and the underlying mechanisms of cafestol-type diterpenoids, which show their potential as functional food and multi-target alternative medicine.

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Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

Section: Biological and Pharmacological Activities Of Cafestol Andmentioning

confidence: 99%

See 1 more Smart Citation

Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Ren

Wang

et al. 2019

IJMS

103

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“…Coffee is a complex beverage containing more than 1000 described phytochemicals responsible for its pleasant flavor, aroma, and health promoters. Several recent scientific publications have described beneficial coffee effects and discussed potential mechanisms of action, including anti-inflammatory [ 59 , 60 ], antiamyloidogenic [ 61 ], antimicrobial, antiglycative [ 62 ], hepatoprotective, antidiabetic, and antiosteoclastogenic effects [ 63 , 64 ].…”

Section: Resultsmentioning

confidence: 99%

Antitumor Effects of Freeze-Dried Robusta Coffee (Coffea canephora) Extracts on Breast Cancer Cell Lines

Nigra

Guimarães

Prucca

et al. 2021

Oxidative Medicine and Cellular Longevity

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Coffee consumption is believed to have chemopreventive and chemotherapeutic effects and to contribute to preventing the development and progression of cancer. However, there is still controversy around these claims. As indicated in our previous works, diet can influence the risk of breast cancer. Intake of coffee is hypothesized to reduce this risk, but current scientific evidence is not conclusive. This work is aimed at studying the effects of Robusta coffee bean extract on cell viability, proliferation, and apoptosis of different human cancers, especially breast cancer cell lines. To this end, cell viability was evaluated by Alamar Blue in 2D and 3D models, the cell cycle by PI, apoptosis by annexin V, mitochondrial morphology, and functionality by mitoTracker, and colony formation capacity by the clonogenic assay. Green and dark coffee extract significantly reduced viability in human breast, colorectal, brain, and bone cancer cells. Coffee anticancer activity was clearly evidenced in MDA-MB-231 (ER-) and MCF-7 (ER+) breast cancer cells but not in the normal breast cell line. In addition, coffee extract induces an increase S phase and a decrease G2/M population in breast cancer cells, affected the mitochondrial morphology, and triggered apoptosis. MDA-MB-231 breast cancer cells lost their clonogenic capacity after treatment. The antitumor activity was demonstrated in both 2D and 3D culture cell models.

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“…Although several positive health benefits have been observed for these compounds, such as anti-inflammatory and chemioprotective properties [4], it was also highlighted that they increase the serum cholesterol levels, especially kahweol and cafestol, both in the free form and as palmitate esters [6,7]. Other studies reported anti-angiogenic [8] and anticancer properties [9].…”

Section: Introductionmentioning

confidence: 99%

Interaction of the Coffee Diterpenes Cafestol and 16-O-Methyl-Cafestol Palmitates with Serum Albumins

Berti

Navarini²,

Guercia³

et al. 2020

IJMS

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The main coffee diterpenes cafestol, kahweol, and 16-O-methylcafestol, present in the bean lipid fraction, are mostly esterified with fatty acids. They are believed to induce dyslipidaemia and hypercholesterolemia when taken with certain types of coffee brews. The study of their binding to serum albumins could help explain their interactions with biologically active xenobiotics. We investigated the interactions occurring between cafestol and 16-O-methylcafestol palmitates with Bovine Serum Albumin (BSA), Human Serum Albumin (HSA), and Fatty Free Human Serum Albumin (ffHSA) by means of circular dichroism and fluorimetry. Circular Dichroism (CD) revealed a slight change (up to 3%) in the secondary structure of fatty-free human albumin in the presence of the diterpene esters, suggesting that the aliphatic chain of the palmitate partly occupies one of the fatty acid sites of the protein. A warfarin displacement experiment was performed to identify the binding site, which is probably close but not coincident with Sudlow site I, as the affinity for warfarin is enhanced. Fluorescence quenching titrations revealed a complex behaviour, with Stern–Volmer constants in the order of 103–104 Lmol−1. A model of the HSA-warfarin-cafestol palmitate complex was obtained by docking, and the most favourable solution was found with the terpene palmitate chain inside the FA4 fatty acid site and the cafestol moiety fronting warfarin at the interface with site I.

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Cafestol, a diterpene molecule found in coffee, induces leukemia cell death

Cited by 28 publications

References 33 publications

Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Cafestol and Kahweol: A Review on Their Bioactivities and Pharmacological Properties

Antitumor Effects of Freeze-Dried Robusta Coffee (Coffea canephora) Extracts on Breast Cancer Cell Lines

Interaction of the Coffee Diterpenes Cafestol and 16-O-Methyl-Cafestol Palmitates with Serum Albumins

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